Emend (Fosaprepitant) (fosaprepitant dimeglumine)

Dosage of fosaprepitant dimeglumine is expressed in terms of fosaprepitant.

Aprepitant is administered orally as capsules (40 mg, 80 mg, 125 mg) or as a powder for oral suspension (125 mg). Aprepitant is also available for IV administration as an injectable emulsion in single-dose vials containing 32 mg/4.4 mL (7.2 mg/mL) or 130 mg/18 mL (7.2 mg/mL).

Fosaprepitant dimeglumine, a prodrug of aprepitant, is available for IV administration as a lyophilized powder for reconstitution in single-dose vials containing 150 mg of fosaprepitant. Fosaprepitant dimeglumine is also available as a ready-to-use injection solution in single-dose vials containing 150 mg/50 mL (3 mg/mL) of fosaprepitant.

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Aprepitant is extensively metabolized in the liver to weakly active metabolites, principally by cytochrome P-450 (CYP) isoenzyme 3A4 and to a lesser extent by CYP1A2 and CYP2C19.

Aprepitant is a substrate, a weak to moderate inhibitor (dose-dependent), and an inducer of CYP3A4. When administered as a 3-day regimen (i.e., 125 mg on day 1 followed by 80 mg on days 2 and 3), aprepitant acts as a moderate inhibitor of CYP3A4. When administered as a single 40-mg dose, aprepitant acts as a weak inhibitor and has not been shown to alter the plasma concentrations of concomitant drugs that are primarily metabolized through CYP3A4. Aprepitant is also an inducer of CYP2C9.

Fosaprepitant, a prodrug of aprepitant, is a weak inhibitor of CYP3A4 when given as a single 150-mg dose, and the weak inhibition of CYP3A4 continues for 2 days after single dose administration. Single-dose fosaprepitant does not induce CYP3A4.

Because fosaprepitant is rapidly metabolized to aprepitant in vivo, interactions reported with aprepitant are expected to occur with fosaprepitant.

There are no contraindication interactions for this drug.

There are no severe interactions for this drug.

There are no moderate interactions for this drug.

*Concomitant use with pimozide.

*Known hypersensitivity to aprepitant, fosaprepitant dimeglumine, or any component of the formulations.

There are no contraindication contraindications for this drug.

There are no severe contraindications for this drug.

There are no moderate contraindications for this drug.

The most common adverse effects (>=3%) with oral aprepitant in adults, when used for the prevention of chemotherapy-induced nausea and vomiting, include fatigue, diarrhea, asthenia, dyspepsia, abdominal pain, hiccups, decreased white blood cell count, dehydration, and increased alanine aminotransferase.

The most common adverse effects (>=3%) with oral aprepitant in pediatric patients, when used for the prevention of chemotherapy-induced nausea and vomiting, include neutropenia, headache, diarrhea, decreased appetite, cough, fatigue, decreased hemoglobin, dizziness, and hiccups.

The most common adverse effects (>=3%) with oral aprepitant in adults, when used for postoperative nausea and vomiting, include constipation and hypotension.

The most common adverse effects (>=2%) with fosaprepitant dimeglumine in adults are fatigue, diarrhea, neutropenia, asthenia, anemia, peripheral neuropathy, leukopenia, dyspepsia, urinary tract infection, and pain in the extremity. Adverse effects in pediatric patients are similar to adults.

The most common adverse effects (>=3%) with single-dose aprepitant for injection (32 mg/4.4 mL) include constipation, fatigue, and headache; and constipation and hypotension with single-dose oral aprepitant.

The most common adverse effects with single-dose fosaprepitant with moderately emetogenic chemotherapy (>=2%) include fatigue, diarrhea, neutropenia, asthenia, anemia, peripheral neuropathy, leukopenia, dyspepsia, urinary tract infection, and pain in the extremity. The most common adverse effects with 3-day oral aprepitant with moderately emetogenic chemotherapy (>=1% and greater than standard therapy) include fatigue and eructation. Adverse effects with single-dose fosaprepitant with highly emetogenic chemotherapy is generally similar to 3-day oral aprepitant; additionally, infusion site reactions (3%) are reported. The most common adverse effects (>=3%) with single-dose aprepitant for injection (130 mg/18 mL) include headache and fatigue.

There are no severe adverse reactions for this drug.

There are no less severe adverse reactions for this drug.

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Safety and efficacy of oral aprepitant or parenteral fosaprepitant dimeglumine for the prevention of nausea and vomiting associated with highly emetogenic chemotherapy (HEC) or moderately emetogenic chemotherapy (MEC) have not been established in pediatric patients <6 months of age.

The safety and efficacy of parenteral aprepitant have not been established in pediatric patients.

The safety and effectiveness of aprepitant capsules have not been established for the prevention of postoperative nausea and vomiting in pediatric patients.

There are insufficient data on the use of aprepitant or fosaprepitant in pregnant women to inform a drug-associated risk. Animal reproduction studies have not demonstrated adverse developmental effects in rats or rabbits exposed during the period of organogenesis. Aprepitant crosses the placenta in animals.

Avoid use of aprepitant injectable emulsions in pregnancy due to the alcohol content.

Aprepitant is distributed into milk in rats; it is not known whether the drug is distributed into milk in humans. The effects of aprepitant on the breast-fed infant or on milk production are also unknown.

Consider the developmental and health benefits of breast-feeding along with the mother's clinical need for aprepitant or fosaprepitant and any potential adverse effects on the breast-fed infant from the drug or from the underlying maternal condition.

In general, use caution when dosing geriatric patients, considering the greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy observed in the elderly.

Clinical experience has not identified differences in efficacy of aprepitant or fosaprepitant in geriatric patients relative to younger patients. No clinically important differences in the pharmacokinetics of oral aprepitant were observed in healthy geriatric patients compared to younger adults.

In general, use caution when dosing geriatric patients, considering the greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy observed in the elderly.